1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
    Autophagy
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  2. HSP
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  3. Tanespimycin

Tanespimycin (Synonyms: 17-AAG; NSC 330507; CP 127374)

製品番号: HY-10211 純度: 99.03%
取扱説明書

Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression.

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Tanespimycin 構造式

Tanespimycin 構造式

CAS 番号 : 75747-14-7

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 79 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 72 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 120 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 300 在庫あり
Estimated Time of Arrival: December 31
200 mg USD 420 在庫あり
Estimated Time of Arrival: December 31
500 mg   お問い合わせ  
1 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 14 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Tanespimycin purchased from MCE. Usage Cited in: Mol Cancer Ther. 2016 Sep;15(9):2107-18.

    Combination of MDV3100 and 17-AAG leads to decreased AR protein level and transcriptional activity. (A&B) LNCaP (A) and C4-2 (B) cells are treated as indicated for 24 hr, followed by IB against AR, PSA and CHIP. (C&D) 22RV1 (C) and MR49F (D) cells are treated as indicated for 24 hr, followed by IB against AR and HSP90. (E) C4-2 cells are treated as indicated for 24 hr, fractionated into cytoplasm and nuclear, followed by IB against AR and Plk1.

    Tanespimycin purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Feb 7;9(2):165.

    Western blot analysis of Hsp70 protein and Hsp90 client proteins IKK and EGFR after 24 h Tan IIA treatment. The Hsp90 inhibitor 17-AAG (10 μM) is included as a positive control

    Tanespimycin purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Mar 27;37(1):70.

    Cells are first treated with commercially available HIF-1α inhibitors, including compounds targeting Top1 (Camptothecin, CPT), Top2 (VP; MX) and HSP90 (17-AAG) as well as 2-ME, and then subjected to Western blotting analysis.

    Tanespimycin purchased from MCE. Usage Cited in: Front Mol Neurosci. 2018 Nov 6;11:401.

    Effects of 17-AAG on neurogenesis 4 weeks after SAH.

    HSP アイソフォーム固有の製品をすべて表示:

    • 生物活性

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    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

    Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90[1][5]. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression[3].

    IC50 & Target

    HSP90

    5 nM (IC50)

    Autophagy

     

    Mitophagy

     

    体外実験

    Tanespimycin causes the degradation of HER2, Akt, and both mutant and wild-type AR and the retinoblastoma-dependent G1 growth arrest of prostate cancer cells. Tanespimycin inhibits prostate cancer cell lines with IC50s ranged from 25-45 nM (LNCaP, 25 nM; LAPC-4, 40 nM; DU-145, 45 nM; and PC-3, 25 nM)[1].
    Tanespimycin (0.1-1 μM) induces a nearly complete loss of ErbB2 on ErbB2-overexpressing breast cancer cells[2]. Tanespimycin inhibits cell growth and induces G2/M cell cycle arrest and apoptosis in CCA cells together with the down-regulation of Bcl-2, Survivin and Cyclin B1, and the up-regulation of cleaved PARP[3].

    体内実験

    Tanespimycin (25-200 mg/kg, i.p.) causes a dose-dependent decline in AR, HER2, and Akt expression in prostate cancer xenografts. Tanespimycin treatment at doses sufficient to induce AR, HER2, and Akt degradation results in the dose-dependent inhibition of androgen-dependent and -independent prostate cancer xenograft growth without toxicity[1].
    Tanespimycin (60 mg/kg) with Rapamycin (30 mg/kg) inhibits A549 and MDA-MB-231 tumor growth and effects tumor cures in MDA-MB-231 tumor-bearing animals by tail vein injection[4].

    臨床実験
    分子量

    585.69

    分子式

    C₃₁H₄₃N₃O₈

    CAS 番号

    75747-14-7

    SMILES

    O=C(C(NC(/C(C)=C/C=C\[[email protected]](OC)[[email protected]](/C(C)=C/[[email protected]@H]([[email protected]]([[email protected]](C[[email protected]@H](C1)C)OC)O)C)OC(N)=O)=O)=CC2=O)C1=C2NCC=C

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 55 mg/mL (93.91 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7074 mL 8.5369 mL 17.0739 mL
    5 mM 0.3415 mL 1.7074 mL 3.4148 mL
    10 mM 0.1707 mL 0.8537 mL 1.7074 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 20 mg/mL (34.15 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (4.27 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are provided by MCE.
    参考文献
    細胞実験
    [1]

    For the Alamar Blue proliferation assay, 2-4×103 cells are plated in 96-well plates. Later (48 h), cells are treated with Tanespimycin for 96 h or 0.01% DMSO as control. On day 4, Alamar Blue viability assay is performed as described elsewhere. IC50 and IC90s are calculated as the doses of Tanespimycin required to inhibit cell growth by 50 and 90%, respectively. Cell cycle distribution is assayed as described previously with a Becton Dickinson fluorescence-activated cell sorter and analyzed by the Cell Cycle Multicycle system.

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [1]

    Tanespimycin is dissolved in an EPL vehicle. To aid in the identification of an optimal dose and schedule, nontumor bearing mice are treated by i.p. injection with 25-200 mg/kg of Tanespimycin 5 days/week for 3 weeks or by the EPL vehicle alone. Serum samples are taken from each group, and equal volumes are pooled on days 5, 10, and 15 of treatment for serum chemistry and liver function analysis. At sacrifice, plasma samples are collected for complete blood count. A gross necropsy is performed on all of the mice, and a complete necropsy, including histopathology, is performed on 1 animal/group.

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    純度: 99.03%

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    Mass   Concentration   Volume   Molecular Weight *
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
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    Keywords:

    Tanespimycin17-AAGNSC 330507CP 127374NSC330507NSC-330507CP127374CP-127374HSPAutophagyMitophagyBacterialApoptosisAntibioticHeat shock proteinsMitochondrial AutophagyARHER2A549MDA-MB-231tumorprostatecancerstk38Inhibitorinhibitorinhibit

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    製品名:
    Tanespimycin
    製品番号:
    HY-10211
    数量:
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